Estetrol, a fetal selective estrogen receptor modulator, acts on the vagina of mice through nuclear ER α activation.

Estetrol, a fetal selective estrogen receptor modulator, acts on the vagina of mice through nuclear ERα activation. Am J Pathol. 2017 Aug 18;: Authors: Benoit T, Valera MC, Fontaine C, Buscato M, Lenfant F, Raymond-Letron I, Tremollieres F, Soulie M, Foidart JM, Game X, Arnal JF Abstract The genito-urinary syndrome of menopause has a negative impact on quality of life of postmenopausal women. The treatment of vulvo-vaginal atrophy (VVA) includes administration of estrogens. However, oral estrogen treatment is controversial due to its potential risks on venous thrombosis and breast cancer. Estetrol (E4) is a natural estrogen synthesized exclusively during pregnancy by the human fetal liver and initially considered as a weak estrogen. However, E4 was recently evaluated in a phase I-II clinical studies and found to act as an oral contraceptive in combination with a progestin, without increasing the level of coagulation factors. We recently showed that E4 stimulates uterine epithelial proliferation through nuclear estrogen receptor (ER) α, but failed to elicit endothelial responses. Here, we first evaluated the morphological and functional impacts of E4 on the vagina of ovariectomized mice and we determined the molecular mechanism mediating these effects. Vaginal epithelial proliferation and lubrication after stimulation were found to increase following E4 chronic treatment. Using the combination of pharmacological and genetic approach...
Source: The American Journal of Pathology - Category: Pathology Authors: Tags: Am J Pathol Source Type: research